onternabez [Ligand Id: 746] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL497392 (HU-308) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| CB1 receptor/Cannabinoid CB1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL218] [GtoPdb: 56] [UniProtKB: P21554] | ||||||||
| ChEMBL | Binding affinity to CB1 receptor | B | 5 | pKi | 10000 | nM | Ki | J Med Chem (2009) 52: 369-378 [PMID:19143566] |
| ChEMBL | Binding affinity to cannabinoid CB1 receptor | B | 5 | pKi | >=10000 | nM | Ki | J Med Chem (2010) 53: 4332-4353 [PMID:20218623] |
| ChEMBL | Displacement of [3H]CP 55940 from human CB1 receptor in cell free system | B | 5 | pKi | 10000 | nM | Ki | Eur J Med Chem (2011) 46: 547-555 [PMID:21183257] |
| CB2 receptor/Cannabinoid CB2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972] | ||||||||
| GtoPdb | - | - | 7.6 | pKi | 25.1 | nM | Ki | Proc Natl Acad Sci USA (1999) 96: 14228-33 [PMID:10588688] |
| ChEMBL | Binding affinity to CB2 receptor | B | 7.64 | pKi | 22.7 | nM | Ki | J Med Chem (2009) 52: 369-378 [PMID:19143566] |
| ChEMBL | Binding affinity to cannabinoid CB2 receptor | B | 7.64 | pKi | 22.7 | nM | Ki | J Med Chem (2010) 53: 4332-4353 [PMID:20218623] |
| ChEMBL | Displacement of [3H]CP 55940 from human CB2 receptor in cell free system | B | 7.64 | pKi | 22.7 | nM | Ki | Eur J Med Chem (2011) 46: 547-555 [PMID:21183257] |
| ChEMBL | Agonist activity at human CB2 receptor expressed in HEK293 cell membranes assessed as induction of [35S]-GTPgammaS binding after 60 mins by liquid scintillation spectrometric method | F | 7.19 | pEC50 | 64.5 | nM | EC50 | J Med Chem (2016) 59: 6753-6771 [PMID:27309150] |
| CB2 receptor/Cannabinoid CB2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2470] [GtoPdb: 57] [UniProtKB: Q9QZN9] | ||||||||
| ChEMBL | Displacement of [3H]HU-243 from rat CB2 receptor expressed in African green monkey COS7 cell membranes after 90 mins | B | 7.64 | pKi | 22.7 | nM | Ki | J Med Chem (2016) 59: 6753-6771 [PMID:27309150] |
| glycine receptor α2 subunit in Human [GtoPdb: 424] [UniProtKB: P23416] | ||||||||
| GtoPdb | - | - | 6 | pIC50 | 1100 | nM | IC50 | |
| glycine receptor α3 subunit in Human [GtoPdb: 425] [UniProtKB: O75311] | ||||||||
| GtoPdb | - | - | 7 | pIC50 | 97 | nM | IC50 | |
ChEMBL data shown on this page come from version 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
